Safety of 6-Nitrobenzo[d]thiazol-2-amineIn 2021, Nath, Rajarshi;Shahar Yar, M.;Pathania, Shelly;Grover, Gourav;Debnath, Biplab;Akhtar, Jawaid Md published 《Synthesis and anticonvulsant evaluation of indoline derivatives of functionalized aryloxadiazole amine and benzothiazole acetamide》. 《Journal of Molecular Structure》published the findings. The article contains the following contents:
A series of I [R = H, 6-Cl, 5-O2N, etc.] and II [R1 = H, 4-MeO, 2-O2N, 4-O2N; R2 = H, 5-Cl, 5-Br] were designed, synthesized and fulfilled structural requirement of pharmacophore and evaluated for anticonvulsant activities using maximal electroshock test (MES), s.c. pentylenetetrazole (scPTZ) seizures and neurotoxicity by motor impairment model in mice. The most active compound I [R = 6-Cl] showed significant anticonvulsant activity against both MES and scPTZ screens and emerged as most effective anticonvulsant compound with median dose of 35.7 mg/kg (MES ED50), 88.15 mg/kg (scPTZ ED50) and toxic dose (TD50) was found to be > 500mg/kg. In-silico studies including mol. docking study were carried out to establish the mol. interaction of potent compound I [R = 6-Cl] in both Na+ channel and GABAA receptors. The prediction of pharmacokinetic parameters and distance mapping of compounds were performed to establish the drug likeness property.6-Nitrobenzo[d]thiazol-2-amine (cas: 6285-57-0) were involved in the experimental procedure.
6-Nitrobenzo[d]thiazol-2-amine(cas:6285-57-0) has been used:
as model analyte for voltammetric determination of electrochemically reducible organic substances;
in the synthesis of 2-methyl-4-nitro-2H-pyrazole-3-carboxylic acid[2-(cyclohexanecarbonylamino)benzothiazol-6-yl]amide derivatives;
in the preparation of push-pull nonlinear optical chromophores containing thiazole and benzothiazole acceptors;
as a base in dye production by diazotation reaction.
Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica